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Assay Detail

CHEMBL4351615

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Binding
Inhibition of FITC-labeled Tat peptide binding to GST-fused PCAF bromodomain (719 to 832 residues) (unknown origin) after 6 hrs by fluorescence polarization assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone acetyltransferase KAT2B (CHEMBL5500)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Huang L, Li H, Li L, Niu L, Seupel R, Wu C, Cheng W, Chen C, Ding B, Brennan PE, Yang S.
J Med Chem (2019) 62 : 4526 -4542
PubMed 30998845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.05 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4070058 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4070058 IC50 = 900.0 nM 6.05